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My CartCAS：85622-93-1
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 85622-93-1 |
| Name | Temozolomide |
| Molecular Formula | C6H6N6O2 |
| Molecular Weight | 194.15 |
| Solubility | Soluble in DMSO ≥10mg/mL |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 630-358-9 |
| MDL | MFCD00866492 |
| SMILES | O=C(C1=C(N2C=N1)N=NN(C)C2=O)N |
| InChIKey | BPEGJWRSRHCHSN-UHFFFAOYSA-N |
| InChI | InChI=1S/C6H6N6O2/c1-11-6(14)12-2-8-3(4(7)13)5(12)9-10-11/h2H,1H3,(H2,7,13) |
| PubChem CID | 5394 |
| Target Point | Autophagy;DNA Alkylator/Crosslinker |
| Passage | Autophagy |
| Background | It is a DNA alkylating agent. It is also a pro-autophagy and pro-apoptosis agent. Has antitumor and antiangiogenic effects. |
| Biological Activity | Temozolomide (NSC 362856; CCRG 81045) 是可口服的用于治疗某些脑癌的DNA烷基化剂。[1-2] |
| In Vitro | 替莫唑胺(TZM)是一种甲基化剂，可穿过血脑屏障，适用于恶性胶质瘤和转移性黑色素瘤。替莫唑胺对肿瘤细胞有效，其特征在于低水平的O6-烷基鸟嘌呤DNA烷基转移酶(OGAT)和功能性错配修复系统(MR)[1]。测定替莫唑胺(TZM)在不同细胞系中的IC50值为14.1至234.6μM，分为两个明显不同的组：IC50值低(100μM)的细胞，包括SF268(147.2±2.1μM)和SK-N-SH细胞(234.6±2.3μM)[2]。 |
| In Vivo | 替莫唑胺(TZM)作为单一药剂，相对于对照，不显著增加mdian存活时间(MST)。值得注意的是，在施用100或200mg/kg替莫唑胺之前立即注射NU1025显著增加了对照组或仅用替莫唑胺治疗的组的寿命。当Temozolomide分次时，使用此方案获得的寿命增加(ILS)高于NU1025与单次注射替莫唑胺时的观察结果(生存曲线的统计比较：颅内NU1025 +替莫唑胺100 mg/kg×2对NU1025)+替莫唑胺200 mg/kg; P = 0.023)[1]。 |
| Cell Experiment | DBA/2(H-2d/H-2d)来源的鼠淋巴瘤细胞系L5178Y在含有10％胎牛血清和抗生素的RPMI-1640中培养。通过用消除PARP活性的浓度(25μM)的8-羟基-2-甲基喹唑啉-4 [3H] -1(NU1025)处理细胞(105细胞/ mL)来获得PARP的抑制。然后将细胞暴露于替莫唑胺(7.5-125μM)并培养3天。通过一式四份计数活细胞来评估细胞生长，并通过DNA含量的流式细胞术分析评估细胞凋亡。通过集落形成试验[1]分析长期存活率。 |
| Animal Experiment | 小鼠[1]雄性B6D2F1(C57BL/6×DBA/2)小鼠用氯胺酮(100mg/kg)和甲苯噻嗪(5mg/kg)在0.9％NaCl溶液(10mL/kg腹膜内)中麻醉。然后使用0.1-mL玻璃微量注射器和27-gauge一次性针头，将L5178Y细胞(104 in 0.03 mL RPMI-1640)颅内注射，通过额骨的中间中间区域至2mm深度。为了评估肿瘤细胞生长，将脑固定在10％磷酸盐缓冲的甲醛中，沿轴平面切割组织切片(5μm)，用苏木精 - 伊红染色，并通过光学显微镜分析。将替莫唑胺溶解于DMSO(40mg/mL)中，用盐水(5mg/mL)稀释，并在肿瘤注射后第2天以100mg/kg或200mg/kg腹膜内给药，通常用于体内临床前研究的剂量。由于替莫唑胺和PARP抑制剂诱导的细胞毒性可通过分次治疗方式改善，因此在选定的组中，总剂量为200 mg/kg替莫唑胺在第2天和第3天分为2剂100 mg/kg。 |
| Data Literature Source | [1]. Tentori L，et al. Combined treatment with temozolomide and poly(ADP-ribose) polymerase inhibitor enhances survival of mice bearing hematologic malignancy at the central nervous system site. Blood. 2002 Mar 15;99(6):2241-4. [2]. Perazzoli G，et al. Temozolomide Resistance in Glioblastoma Cell Lines: Implication of MGMT，MMR，P-Glycoprotein and CD133 Expression. PLoS One. 2015 Oct 8;10(10):e0140131 |
| Unit | Bottle |
| Specification | 10mg 10mM*1mL in DMSO 50mg 100mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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